Details of the Target

General Information of Target

Target ID LDTP10346
Target Name Aurora kinase B (AURKB)
Gene Name AURKB
Gene ID 9212
Synonyms
AIK2; AIM1; AIRK2; ARK2; STK1; STK12; STK5; Aurora kinase B; EC 2.7.11.1; Aurora 1; Aurora- and IPL1-like midbody-associated protein 1; AIM-1; Aurora/IPL1-related kinase 2; ARK-2; Aurora-related kinase 2; STK-1; Serine/threonine-protein kinase 12; Serine/threonine-protein kinase 5; Serine/threonine-protein kinase aurora-B
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MLVCYSVLACEILWDLPCSIMGSPLGHFTWDKYLKETCSVPAPVHCFKQSYTPPSNEFKI
SMKLEAQDPRNTTSTCIATVVGLTGARLRLRLDGSDNKNDFWRLVDSAEIQPIGNCEKNG
GMLQPPLGFRLNASSWPMFLLKTLNGAEMAPIRIFHKEPPSPSHNFFKMGMKLEAVDRKN
PHFICPATIGEVRGSEVLVTFDGWRGAFDYWCRFDSRDIFPVGWCSLTGDNLQPPGTKVV
IPKNPYPASDVNTEKPSIHSSTKTVLEHQPGQRGRKPGKKRGRTPKTLISHPISAPSKTA
EPLKFPKKRGPKPGSKRKPRTLLNPPPASPTTSTPEPDTSTVPQDAATIPSSAMQAPTVC
IYLNKNGSTGPHLDKKKVQQLPDHFGPARASVVLQQAVQACIDCAYHQKTVFSFLKQGHG
GEVISAVFDREQHTLNLPAVNSITYVLRFLEKLCHNLRSDNLFGNQPFTQTHLSLTAIEY
SHSHDRYLPGETFVLGNSLARSLEPHSDSMDSASNPTNLVSTSQRHRPLLSSCGLPPSTA
SAVRRLCSRGVLKGSNERRDMESFWKLNRSPGSDRYLESRDASRLSGRDPSSWTVEDVMQ
FVREADPQLGPHADLFRKHEIDGKALLLLRSDMMMKYMGLKLGPALKLSYHIDRLKQGKF
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Ser/Thr protein kinase family, Aurora subfamily
Subcellular location
Nucleus
Function
Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Involved in the bipolar attachment of spindle microtubules to kinetochores and is a key regulator for the onset of cytokinesis during mitosis. Required for central/midzone spindle assembly and cleavage furrow formation. Key component of the cytokinesis checkpoint, a process required to delay abscission to prevent both premature resolution of intercellular chromosome bridges and accumulation of DNA damage: phosphorylates CHMP4C, leading to retain abscission-competent VPS4 (VPS4A and/or VPS4B) at the midbody ring until abscission checkpoint signaling is terminated at late cytokinesis. AURKB phosphorylates the CPC complex subunits BIRC5/survivin, CDCA8/borealin and INCENP. Phosphorylation of INCENP leads to increased AURKB activity. Other known AURKB substrates involved in centromeric functions and mitosis are CENPA, DES/desmin, GPAF, KIF2C, NSUN2, RACGAP1, SEPTIN1, VIM/vimentin, HASPIN, and histone H3. A positive feedback loop involving HASPIN and AURKB contributes to localization of CPC to centromeres. Phosphorylation of VIM controls vimentin filament segregation in cytokinetic process, whereas histone H3 is phosphorylated at 'Ser-10' and 'Ser-28' during mitosis (H3S10ph and H3S28ph, respectively). AURKB is also required for kinetochore localization of BUB1 and SGO1. Phosphorylation of p53/TP53 negatively regulates its transcriptional activity. Key regulator of active promoters in resting B- and T-lymphocytes: acts by mediating phosphorylation of H3S28ph at active promoters in resting B-cells, inhibiting RNF2/RING1B-mediated ubiquitination of histone H2A and enhancing binding and activity of the USP16 deubiquitinase at transcribed genes. Acts as an inhibitor of CGAS during mitosis: catalyzes phosphorylation of the N-terminus of CGAS during the G2-M transition, blocking CGAS liquid phase separation and activation, and thereby preventing CGAS-induced autoimmunity. Phosphorylates KRT5 during anaphase and telophase.
TTD ID
T46781
Uniprot ID
Q96GD4
DrugMap ID
TT5LS6T
Ensemble ID
ENST00000316199.10
HGNC ID
HGNC:11390
ChEMBL ID
CHEMBL2185

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CORL23 SNV: p.G247R .
HS839T Deletion: p.L307AfsTer4 DBIA    Probe Info 
IGR37 SNV: p.F88L DBIA    Probe Info 
IGR39 SNV: p.F88L DBIA    Probe Info 
WM115 SNV: p.Ter345RextTer? DBIA    Probe Info 
WM2664 SNV: p.Ter345RextTer? .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 24 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
STPyne
 Probe Info  		K211(8.33); K87(0.75)  LDD0277  [2]
BTD
 Probe Info  		C170(0.87)  LDD2125  [3]
MCL-14
 Probe Info  		1.70  LDD0050  [4]
EA-probe
 Probe Info  		N.A.  LDD0440  [5]
HHS-482
 Probe Info  		Y92(2.98)  LDD0285  [6]
HHS-475
 Probe Info  		Y92(0.80)  LDD0264  [7]
DBIA
 Probe Info  		C170(1.70)  LDD0080  [8]
ATP probe
 Probe Info  		K87(0.00); K202(0.00); K231(0.00)  LDD0199  [9]
4-Iodoacetamidophenylacetylene
 Probe Info  		C170(0.00); C191(0.00); C234(0.00)  LDD0038  [10]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [11]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [12]
Lodoacetamide azide
 Probe Info  		C170(0.00); C191(0.00); C234(0.00)  LDD0037  [10]
TFBX
 Probe Info  		N.A.  LDD0027  [13]
Compound 10
 Probe Info  		N.A.  LDD2216  [14]
IPM
 Probe Info  		N.A.  LDD0147  [13]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [15]
1c-yne
 Probe Info  		N.A.  LDD0228  [16]
Acrolein
 Probe Info  		C234(0.00); C170(0.00)  LDD0217  [17]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [17]
Methacrolein
 Probe Info  		N.A.  LDD0218  [17]
AOyne
 Probe Info  		15.00  LDD0443  [18]
NAIA_5
 Probe Info  		N.A.  LDD2223  [19]
HHS-465
 Probe Info  		N.A.  LDD2240  [20]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Staurosporine capture compound
 Probe Info  		N.A.  LDD0083  [21]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C170(0.96); C234(0.98)  LDD0531  [8]
 LDCM0215  AC10 HCT 116 C234(1.12)  LDD0532  [8]
 LDCM0216  AC100 HCT 116 C234(1.21)  LDD0533  [8]
 LDCM0217  AC101 HCT 116 C234(1.02)  LDD0534  [8]
 LDCM0218  AC102 HCT 116 C234(1.07)  LDD0535  [8]
 LDCM0219  AC103 HCT 116 C234(1.44)  LDD0536  [8]
 LDCM0220  AC104 HCT 116 C234(1.08)  LDD0537  [8]
 LDCM0221  AC105 HCT 116 C234(1.20)  LDD0538  [8]
 LDCM0222  AC106 HCT 116 C234(1.40)  LDD0539  [8]
 LDCM0223  AC107 HCT 116 C234(0.86)  LDD0540  [8]
 LDCM0224  AC108 HCT 116 C234(1.21)  LDD0541  [8]
 LDCM0225  AC109 HCT 116 C234(1.08)  LDD0542  [8]
 LDCM0226  AC11 HCT 116 C234(1.44)  LDD0543  [8]
 LDCM0227  AC110 HCT 116 C234(1.03)  LDD0544  [8]
 LDCM0228  AC111 HCT 116 C234(1.65)  LDD0545  [8]
 LDCM0229  AC112 HCT 116 C234(1.06)  LDD0546  [8]
 LDCM0230  AC113 HCT 116 C170(0.95); C234(0.76)  LDD0547  [8]
 LDCM0231  AC114 HCT 116 C170(0.94); C234(1.00)  LDD0548  [8]
 LDCM0232  AC115 HCT 116 C170(1.05); C234(1.13)  LDD0549  [8]
 LDCM0233  AC116 HCT 116 C170(1.08); C234(1.31)  LDD0550  [8]
 LDCM0234  AC117 HCT 116 C170(1.19); C234(1.14)  LDD0551  [8]
 LDCM0235  AC118 HCT 116 C170(1.06); C234(0.89)  LDD0552  [8]
 LDCM0236  AC119 HCT 116 C170(0.93); C234(0.98)  LDD0553  [8]
 LDCM0237  AC12 HCT 116 C234(1.07)  LDD0554  [8]
 LDCM0238  AC120 HCT 116 C170(1.02); C234(1.18)  LDD0555  [8]
 LDCM0239  AC121 HCT 116 C170(1.00); C234(0.80)  LDD0556  [8]
 LDCM0240  AC122 HCT 116 C170(1.00); C234(0.98)  LDD0557  [8]
 LDCM0241  AC123 HCT 116 C170(0.94); C234(0.90)  LDD0558  [8]
 LDCM0242  AC124 HCT 116 C170(0.96); C234(0.84)  LDD0559  [8]
 LDCM0243  AC125 HCT 116 C170(0.92); C234(1.10)  LDD0560  [8]
 LDCM0244  AC126 HCT 116 C170(1.01); C234(1.01)  LDD0561  [8]
 LDCM0245  AC127 HCT 116 C170(0.90); C234(1.04)  LDD0562  [8]
 LDCM0246  AC128 HCT 116 C234(0.85)  LDD0563  [8]
 LDCM0247  AC129 HCT 116 C234(0.93)  LDD0564  [8]
 LDCM0249  AC130 HCT 116 C234(1.09)  LDD0566  [8]
 LDCM0250  AC131 HCT 116 C234(1.01)  LDD0567  [8]
 LDCM0251  AC132 HCT 116 C234(1.06)  LDD0568  [8]
 LDCM0252  AC133 HCT 116 C234(1.07)  LDD0569  [8]
 LDCM0253  AC134 HCT 116 C234(1.33)  LDD0570  [8]
 LDCM0254  AC135 HCT 116 C234(1.08)  LDD0571  [8]
 LDCM0255  AC136 HCT 116 C234(1.14)  LDD0572  [8]
 LDCM0256  AC137 HCT 116 C234(1.09)  LDD0573  [8]
 LDCM0257  AC138 HCT 116 C234(1.76)  LDD0574  [8]
 LDCM0258  AC139 HCT 116 C234(1.53)  LDD0575  [8]
 LDCM0259  AC14 HCT 116 C234(1.20)  LDD0576  [8]
 LDCM0260  AC140 HCT 116 C234(1.40)  LDD0577  [8]
 LDCM0261  AC141 HCT 116 C234(1.37)  LDD0578  [8]
 LDCM0262  AC142 HCT 116 C234(1.11)  LDD0579  [8]
 LDCM0263  AC143 HCT 116 C234(1.09)  LDD0580  [8]
 LDCM0264  AC144 HCT 116 C234(1.04)  LDD0581  [8]
 LDCM0265  AC145 HCT 116 C234(0.90)  LDD0582  [8]
 LDCM0266  AC146 HCT 116 C234(0.99)  LDD0583  [8]
 LDCM0267  AC147 HCT 116 C234(0.99)  LDD0584  [8]
 LDCM0268  AC148 HCT 116 C234(1.17)  LDD0585  [8]
 LDCM0269  AC149 HCT 116 C234(1.03)  LDD0586  [8]
 LDCM0270  AC15 HCT 116 C234(1.08)  LDD0587  [8]
 LDCM0271  AC150 HCT 116 C234(1.01)  LDD0588  [8]
 LDCM0272  AC151 HCT 116 C234(1.07)  LDD0589  [8]
 LDCM0273  AC152 HCT 116 C234(0.93)  LDD0590  [8]
 LDCM0274  AC153 HCT 116 C234(1.28)  LDD0591  [8]
 LDCM0621  AC154 HCT 116 C234(1.10)  LDD2158  [8]
 LDCM0622  AC155 HCT 116 C234(1.12)  LDD2159  [8]
 LDCM0623  AC156 HCT 116 C234(1.12)  LDD2160  [8]
 LDCM0624  AC157 HCT 116 C234(0.94)  LDD2161  [8]
 LDCM0276  AC17 HCT 116 C234(1.06); C170(1.16)  LDD0593  [8]
 LDCM0277  AC18 HCT 116 C234(1.13); C170(1.20)  LDD0594  [8]
 LDCM0278  AC19 HCT 116 C234(1.07); C170(1.30)  LDD0595  [8]
 LDCM0279  AC2 HCT 116 C170(0.93); C234(1.11)  LDD0596  [8]
 LDCM0280  AC20 HCT 116 C234(0.98); C170(1.20)  LDD0597  [8]
 LDCM0281  AC21 HCT 116 C234(1.00); C170(1.38)  LDD0598  [8]
 LDCM0282  AC22 HCT 116 C234(1.06); C170(1.25)  LDD0599  [8]
 LDCM0283  AC23 HCT 116 C234(0.90); C170(1.28)  LDD0600  [8]
 LDCM0284  AC24 HCT 116 C234(1.04); C170(1.22)  LDD0601  [8]
 LDCM0285  AC25 HCT 116 C234(1.30); C170(1.52)  LDD0602  [8]
 LDCM0286  AC26 HCT 116 C234(1.29); C170(1.52)  LDD0603  [8]
 LDCM0287  AC27 HCT 116 C234(1.17); C170(2.26)  LDD0604  [8]
 LDCM0288  AC28 HCT 116 C170(1.63); C234(2.14)  LDD0605  [8]
 LDCM0289  AC29 HCT 116 C170(1.75); C234(1.79)  LDD0606  [8]
 LDCM0290  AC3 HCT 116 C170(1.03); C234(1.05)  LDD0607  [8]
 LDCM0291  AC30 HCT 116 C170(1.26); C234(1.34)  LDD0608  [8]
 LDCM0292  AC31 HCT 116 C170(1.33); C234(1.41)  LDD0609  [8]
 LDCM0293  AC32 HCT 116 C234(1.18); C170(1.63)  LDD0610  [8]
 LDCM0294  AC33 HCT 116 C234(1.43); C170(1.78)  LDD0611  [8]
 LDCM0295  AC34 HCT 116 C234(1.76); C170(1.79)  LDD0612  [8]
 LDCM0296  AC35 HCT 116 C170(0.96); C234(1.09)  LDD0613  [8]
 LDCM0297  AC36 HCT 116 C234(0.97); C170(0.98)  LDD0614  [8]
 LDCM0298  AC37 HCT 116 C170(0.90); C234(1.09)  LDD0615  [8]
 LDCM0299  AC38 HCT 116 C170(0.94); C234(1.27)  LDD0616  [8]
 LDCM0300  AC39 HCT 116 C170(1.03); C234(1.26)  LDD0617  [8]
 LDCM0301  AC4 HCT 116 C170(1.12); C234(1.14)  LDD0618  [8]
 LDCM0302  AC40 HCT 116 C170(1.08); C234(1.33)  LDD0619  [8]
 LDCM0303  AC41 HCT 116 C170(1.04); C234(1.56)  LDD0620  [8]
 LDCM0304  AC42 HCT 116 C170(0.90); C234(1.54)  LDD0621  [8]
 LDCM0305  AC43 HCT 116 C170(0.88); C234(1.03)  LDD0622  [8]
 LDCM0306  AC44 HCT 116 C170(0.97); C234(1.26)  LDD0623  [8]
 LDCM0307  AC45 HCT 116 C170(0.90); C234(1.41)  LDD0624  [8]
 LDCM0308  AC46 HCT 116 C170(1.07); C234(1.29)  LDD0625  [8]
 LDCM0309  AC47 HCT 116 C170(1.09); C234(1.24)  LDD0626  [8]
 LDCM0310  AC48 HCT 116 C170(0.99); C234(1.13)  LDD0627  [8]
 LDCM0311  AC49 HCT 116 C170(1.28); C234(1.34)  LDD0628  [8]
 LDCM0312  AC5 HCT 116 C234(1.01); C170(1.15)  LDD0629  [8]
 LDCM0313  AC50 HCT 116 C170(0.99); C234(1.23)  LDD0630  [8]
 LDCM0314  AC51 HCT 116 C170(1.03); C234(1.16)  LDD0631  [8]
 LDCM0315  AC52 HCT 116 C234(1.04); C170(1.23)  LDD0632  [8]
 LDCM0316  AC53 HCT 116 C170(1.04); C234(1.16)  LDD0633  [8]
 LDCM0317  AC54 HCT 116 C234(1.17); C170(1.18)  LDD0634  [8]
 LDCM0318  AC55 HCT 116 C170(1.10); C234(1.15)  LDD0635  [8]
 LDCM0319  AC56 HCT 116 C170(0.93); C234(1.15)  LDD0636  [8]
 LDCM0320  AC57 HCT 116 C170(1.37); C234(1.50)  LDD0637  [8]
 LDCM0321  AC58 HCT 116 C170(1.08); C234(1.55)  LDD0638  [8]
 LDCM0322  AC59 HCT 116 C170(1.38); C234(1.77)  LDD0639  [8]
 LDCM0323  AC6 HCT 116 C234(1.15)  LDD0640  [8]
 LDCM0324  AC60 HCT 116 C170(1.36); C234(1.55)  LDD0641  [8]
 LDCM0325  AC61 HCT 116 C234(1.33); C170(1.38)  LDD0642  [8]
 LDCM0326  AC62 HCT 116 C170(1.35); C234(1.45)  LDD0643  [8]
 LDCM0327  AC63 HCT 116 C170(1.14); C234(1.52)  LDD0644  [8]
 LDCM0328  AC64 HCT 116 C170(1.40); C234(1.75)  LDD0645  [8]
 LDCM0329  AC65 HCT 116 C170(1.32); C234(1.70)  LDD0646  [8]
 LDCM0330  AC66 HCT 116 C170(1.32); C234(1.63)  LDD0647  [8]
 LDCM0331  AC67 HCT 116 C170(1.48); C234(1.71)  LDD0648  [8]
 LDCM0332  AC68 HCT 116 C234(0.92)  LDD0649  [8]
 LDCM0333  AC69 HCT 116 C234(0.77)  LDD0650  [8]
 LDCM0334  AC7 HCT 116 C234(0.99)  LDD0651  [8]
 LDCM0335  AC70 HCT 116 C234(1.00)  LDD0652  [8]
 LDCM0336  AC71 HCT 116 C234(0.73)  LDD0653  [8]
 LDCM0337  AC72 HCT 116 C234(1.33)  LDD0654  [8]
 LDCM0338  AC73 HCT 116 C234(1.16)  LDD0655  [8]
 LDCM0339  AC74 HCT 116 C234(0.90)  LDD0656  [8]
 LDCM0340  AC75 HCT 116 C234(1.08)  LDD0657  [8]
 LDCM0341  AC76 HCT 116 C234(1.02)  LDD0658  [8]
 LDCM0342  AC77 HCT 116 C234(1.13)  LDD0659  [8]
 LDCM0343  AC78 HCT 116 C234(0.82)  LDD0660  [8]
 LDCM0344  AC79 HCT 116 C234(1.13)  LDD0661  [8]
 LDCM0345  AC8 HCT 116 C234(1.08)  LDD0662  [8]
 LDCM0346  AC80 HCT 116 C234(1.04)  LDD0663  [8]
 LDCM0347  AC81 HCT 116 C234(0.76)  LDD0664  [8]
 LDCM0348  AC82 HCT 116 C234(1.05)  LDD0665  [8]
 LDCM0349  AC83 HCT 116 C170(0.91); C234(1.57)  LDD0666  [8]
 LDCM0350  AC84 HCT 116 C170(1.06); C234(1.19)  LDD0667  [8]
 LDCM0351  AC85 HCT 116 C234(1.19); C170(1.31)  LDD0668  [8]
 LDCM0352  AC86 HCT 116 C234(1.09); C170(1.16)  LDD0669  [8]
 LDCM0353  AC87 HCT 116 C234(0.79); C170(1.02)  LDD0670  [8]
 LDCM0354  AC88 HCT 116 C170(0.97); C234(0.99)  LDD0671  [8]
 LDCM0355  AC89 HCT 116 C170(1.08); C234(1.08)  LDD0672  [8]
 LDCM0357  AC90 HCT 116 C234(0.94); C170(1.07)  LDD0674  [8]
 LDCM0358  AC91 HCT 116 C170(1.24); C234(1.50)  LDD0675  [8]
 LDCM0359  AC92 HCT 116 C170(1.18); C234(1.18)  LDD0676  [8]
 LDCM0360  AC93 HCT 116 C170(0.95); C234(1.09)  LDD0677  [8]
 LDCM0361  AC94 HCT 116 C234(1.13); C170(1.24)  LDD0678  [8]
 LDCM0362  AC95 HCT 116 C234(0.91); C170(1.02)  LDD0679  [8]
 LDCM0363  AC96 HCT 116 C170(1.12); C234(1.44)  LDD0680  [8]
 LDCM0364  AC97 HCT 116 C170(1.21); C234(1.23)  LDD0681  [8]
 LDCM0365  AC98 HCT 116 C234(1.44)  LDD0682  [8]
 LDCM0366  AC99 HCT 116 C234(1.01)  LDD0683  [8]
 LDCM0248  AKOS034007472 HCT 116 C234(0.94)  LDD0565  [8]
 LDCM0356  AKOS034007680 HCT 116 C234(1.15)  LDD0673  [8]
 LDCM0275  AKOS034007705 HCT 116 C234(1.40)  LDD0592  [8]
 LDCM0156  Aniline NCI-H1299 13.11  LDD0403  [1]
 LDCM0367  CL1 HCT 116 C170(1.02); C234(1.03)  LDD0684  [8]
 LDCM0368  CL10 HCT 116 C234(1.05); C170(1.25)  LDD0685  [8]
 LDCM0369  CL100 HCT 116 C170(1.09); C234(1.20)  LDD0686  [8]
 LDCM0370  CL101 HCT 116 C234(1.00)  LDD0687  [8]
 LDCM0371  CL102 HCT 116 C234(0.95)  LDD0688  [8]
 LDCM0372  CL103 HCT 116 C234(0.84)  LDD0689  [8]
 LDCM0373  CL104 HCT 116 C234(0.95)  LDD0690  [8]
 LDCM0374  CL105 HCT 116 C234(0.95); C170(1.10)  LDD0691  [8]
 LDCM0375  CL106 HCT 116 C234(1.00); C170(1.64)  LDD0692  [8]
 LDCM0376  CL107 HCT 116 C234(1.04); C170(1.42)  LDD0693  [8]
 LDCM0377  CL108 HCT 116 C234(1.05); C170(1.37)  LDD0694  [8]
 LDCM0378  CL109 HCT 116 C234(1.11); C170(1.45)  LDD0695  [8]
 LDCM0379  CL11 HCT 116 C170(0.89); C234(1.13)  LDD0696  [8]
 LDCM0380  CL110 HCT 116 C234(1.00); C170(1.30)  LDD0697  [8]
 LDCM0381  CL111 HCT 116 C234(1.17); C170(1.23)  LDD0698  [8]
 LDCM0382  CL112 HCT 116 C234(0.88); C170(1.29)  LDD0699  [8]
 LDCM0383  CL113 HCT 116 C234(1.09); C170(1.53)  LDD0700  [8]
 LDCM0384  CL114 HCT 116 C234(1.47); C170(1.57)  LDD0701  [8]
 LDCM0385  CL115 HCT 116 C234(1.27); C170(2.09)  LDD0702  [8]
 LDCM0386  CL116 HCT 116 C234(1.39); C170(1.67)  LDD0703  [8]
 LDCM0387  CL117 HCT 116 C170(0.90); C234(1.52)  LDD0704  [8]
 LDCM0388  CL118 HCT 116 C170(0.91); C234(1.25)  LDD0705  [8]
 LDCM0389  CL119 HCT 116 C170(0.91); C234(1.19)  LDD0706  [8]
 LDCM0390  CL12 HCT 116 C234(0.96); C170(1.22)  LDD0707  [8]
 LDCM0391  CL120 HCT 116 C170(0.99); C234(1.22)  LDD0708  [8]
 LDCM0392  CL121 HCT 116 C234(1.02); C170(1.16)  LDD0709  [8]
 LDCM0393  CL122 HCT 116 C170(1.16); C234(1.20)  LDD0710  [8]
 LDCM0394  CL123 HCT 116 C170(0.89); C234(0.95)  LDD0711  [8]
 LDCM0395  CL124 HCT 116 C170(1.05); C234(1.23)  LDD0712  [8]
 LDCM0396  CL125 HCT 116 C170(1.10); C234(1.16)  LDD0713  [8]
 LDCM0397  CL126 HCT 116 C170(1.06); C234(1.08)  LDD0714  [8]
 LDCM0398  CL127 HCT 116 C170(1.06); C234(1.38)  LDD0715  [8]
 LDCM0399  CL128 HCT 116 C170(1.16); C234(1.29)  LDD0716  [8]
 LDCM0400  CL13 HCT 116 C234(1.02); C170(1.14)  LDD0717  [8]
 LDCM0401  CL14 HCT 116 C234(0.99); C170(1.16)  LDD0718  [8]
 LDCM0402  CL15 HCT 116 C170(0.95); C234(0.96)  LDD0719  [8]
 LDCM0403  CL16 HCT 116 C170(0.93); C234(1.10)  LDD0720  [8]
 LDCM0404  CL17 HCT 116 C234(0.97); C170(1.03)  LDD0721  [8]
 LDCM0405  CL18 HCT 116 C234(1.02); C170(1.10)  LDD0722  [8]
 LDCM0406  CL19 HCT 116 C234(0.99); C170(1.18)  LDD0723  [8]
 LDCM0407  CL2 HCT 116 C170(1.02); C234(1.10)  LDD0724  [8]
 LDCM0408  CL20 HCT 116 C234(1.10); C170(1.34)  LDD0725  [8]
 LDCM0409  CL21 HCT 116 C234(1.01); C170(1.06)  LDD0726  [8]
 LDCM0410  CL22 HCT 116 C234(0.99); C170(1.04)  LDD0727  [8]
 LDCM0411  CL23 HCT 116 C234(1.06); C170(1.12)  LDD0728  [8]
 LDCM0412  CL24 HCT 116 C234(1.04); C170(1.13)  LDD0729  [8]
 LDCM0413  CL25 HCT 116 C170(1.07); C234(1.07)  LDD0730  [8]
 LDCM0414  CL26 HCT 116 C170(1.14); C234(1.05)  LDD0731  [8]
 LDCM0415  CL27 HCT 116 C170(1.26); C234(0.98)  LDD0732  [8]
 LDCM0416  CL28 HCT 116 C170(0.97); C234(1.07)  LDD0733  [8]
 LDCM0417  CL29 HCT 116 C170(1.10); C234(1.18)  LDD0734  [8]
 LDCM0418  CL3 HCT 116 C170(1.32); C234(0.89)  LDD0735  [8]
 LDCM0419  CL30 HCT 116 C170(0.92); C234(1.03)  LDD0736  [8]
 LDCM0420  CL31 HCT 116 C170(0.89); C234(1.07)  LDD0737  [8]
 LDCM0421  CL32 HCT 116 C170(1.04); C234(1.11)  LDD0738  [8]
 LDCM0422  CL33 HCT 116 C170(0.90); C234(1.32)  LDD0739  [8]
 LDCM0423  CL34 HCT 116 C170(0.99); C234(1.51)  LDD0740  [8]
 LDCM0424  CL35 HCT 116 C170(1.08); C234(1.47)  LDD0741  [8]
 LDCM0425  CL36 HCT 116 C170(0.93); C234(1.39)  LDD0742  [8]
 LDCM0426  CL37 HCT 116 C170(1.06); C234(1.44)  LDD0743  [8]
 LDCM0428  CL39 HCT 116 C170(1.07); C234(1.40)  LDD0745  [8]
 LDCM0429  CL4 HCT 116 C170(0.84); C234(1.00)  LDD0746  [8]
 LDCM0430  CL40 HCT 116 C170(0.99); C234(1.41)  LDD0747  [8]
 LDCM0431  CL41 HCT 116 C170(0.90); C234(1.46)  LDD0748  [8]
 LDCM0432  CL42 HCT 116 C170(0.91); C234(1.60)  LDD0749  [8]
 LDCM0433  CL43 HCT 116 C170(1.01); C234(1.59)  LDD0750  [8]
 LDCM0434  CL44 HCT 116 C170(1.13); C234(1.45)  LDD0751  [8]
 LDCM0435  CL45 HCT 116 C170(1.15); C234(1.64)  LDD0752  [8]
 LDCM0436  CL46 HCT 116 C170(1.03); C234(0.90)  LDD0753  [8]
 LDCM0437  CL47 HCT 116 C170(0.97); C234(0.78)  LDD0754  [8]
 LDCM0438  CL48 HCT 116 C170(1.13); C234(0.81)  LDD0755  [8]
 LDCM0439  CL49 HCT 116 C170(0.94); C234(0.97)  LDD0756  [8]
 LDCM0440  CL5 HCT 116 C170(1.07); C234(0.90)  LDD0757  [8]
 LDCM0441  CL50 HCT 116 C170(1.03); C234(0.82)  LDD0758  [8]
 LDCM0442  CL51 HCT 116 C170(1.11); C234(0.85)  LDD0759  [8]
 LDCM0443  CL52 HCT 116 C170(1.11); C234(1.24)  LDD0760  [8]
 LDCM0444  CL53 HCT 116 C170(1.08); C234(0.75)  LDD0761  [8]
 LDCM0445  CL54 HCT 116 C170(1.04); C234(0.84)  LDD0762  [8]
 LDCM0446  CL55 HCT 116 C170(1.02); C234(0.76)  LDD0763  [8]
 LDCM0447  CL56 HCT 116 C170(1.01); C234(0.78)  LDD0764  [8]
 LDCM0448  CL57 HCT 116 C170(0.96); C234(0.88)  LDD0765  [8]
 LDCM0449  CL58 HCT 116 C170(1.13); C234(0.92)  LDD0766  [8]
 LDCM0450  CL59 HCT 116 C170(1.20); C234(0.88)  LDD0767  [8]
 LDCM0451  CL6 HCT 116 C170(1.11); C234(1.05)  LDD0768  [8]
 LDCM0452  CL60 HCT 116 C170(1.11); C234(0.83)  LDD0769  [8]
 LDCM0453  CL61 HCT 116 C170(0.90)  LDD0770  [8]
 LDCM0454  CL62 HCT 116 C170(1.04)  LDD0771  [8]
 LDCM0455  CL63 HCT 116 C170(1.01)  LDD0772  [8]
 LDCM0456  CL64 HCT 116 C170(0.97)  LDD0773  [8]
 LDCM0457  CL65 HCT 116 C170(1.16)  LDD0774  [8]
 LDCM0458  CL66 HCT 116 C170(1.08)  LDD0775  [8]
 LDCM0459  CL67 HCT 116 C170(1.06)  LDD0776  [8]
 LDCM0460  CL68 HCT 116 C170(0.97)  LDD0777  [8]
 LDCM0461  CL69 HCT 116 C170(1.00)  LDD0778  [8]
 LDCM0462  CL7 HCT 116 C170(1.13); C234(0.94)  LDD0779  [8]
 LDCM0463  CL70 HCT 116 C170(0.81)  LDD0780  [8]
 LDCM0464  CL71 HCT 116 C170(0.95)  LDD0781  [8]
 LDCM0465  CL72 HCT 116 C170(1.00)  LDD0782  [8]
 LDCM0466  CL73 HCT 116 C170(0.96)  LDD0783  [8]
 LDCM0467  CL74 HCT 116 C170(1.04)  LDD0784  [8]
 LDCM0469  CL76 HCT 116 C234(1.06)  LDD0786  [8]
 LDCM0470  CL77 HCT 116 C234(0.88)  LDD0787  [8]
 LDCM0471  CL78 HCT 116 C234(1.08)  LDD0788  [8]
 LDCM0472  CL79 HCT 116 C234(1.25)  LDD0789  [8]
 LDCM0473  CL8 HCT 116 C170(0.85); C234(1.16)  LDD0790  [8]
 LDCM0474  CL80 HCT 116 C234(0.93)  LDD0791  [8]
 LDCM0475  CL81 HCT 116 C234(1.10)  LDD0792  [8]
 LDCM0476  CL82 HCT 116 C234(1.29)  LDD0793  [8]
 LDCM0477  CL83 HCT 116 C234(1.23)  LDD0794  [8]
 LDCM0478  CL84 HCT 116 C234(1.58)  LDD0795  [8]
 LDCM0479  CL85 HCT 116 C234(0.94)  LDD0796  [8]
 LDCM0480  CL86 HCT 116 C234(0.95)  LDD0797  [8]
 LDCM0481  CL87 HCT 116 C234(1.06)  LDD0798  [8]
 LDCM0482  CL88 HCT 116 C234(1.22)  LDD0799  [8]
 LDCM0483  CL89 HCT 116 C234(1.62)  LDD0800  [8]
 LDCM0484  CL9 HCT 116 C170(1.19); C234(1.12)  LDD0801  [8]
 LDCM0485  CL90 HCT 116 C234(0.92)  LDD0802  [8]
 LDCM0486  CL91 HCT 116 C170(0.78); C234(1.02)  LDD0803  [8]
 LDCM0487  CL92 HCT 116 C170(0.83); C234(1.10)  LDD0804  [8]
 LDCM0488  CL93 HCT 116 C170(0.87); C234(1.11)  LDD0805  [8]
 LDCM0489  CL94 HCT 116 C170(0.97); C234(1.14)  LDD0806  [8]
 LDCM0490  CL95 HCT 116 C170(0.83); C234(1.21)  LDD0807  [8]
 LDCM0491  CL96 HCT 116 C170(1.00); C234(1.17)  LDD0808  [8]
 LDCM0492  CL97 HCT 116 C170(1.07); C234(1.25)  LDD0809  [8]
 LDCM0493  CL98 HCT 116 C170(0.93); C234(1.21)  LDD0810  [8]
 LDCM0494  CL99 HCT 116 C170(0.94); C234(1.20)  LDD0811  [8]
 LDCM0495  E2913 HEK-293T C234(1.03); C191(0.97)  LDD1698  [22]
 LDCM0175  Ethacrynic acid HeLa N.A.  LDD0440  [5]
 LDCM0625  F8 Ramos C170(1.25)  LDD2187  [23]
 LDCM0572  Fragment10 Ramos C170(1.03)  LDD2189  [23]
 LDCM0574  Fragment12 Ramos C170(1.28)  LDD2191  [23]
 LDCM0576  Fragment14 Ramos C170(1.16); C234(1.25)  LDD2193  [23]
 LDCM0579  Fragment20 Ramos C170(1.26)  LDD2194  [23]
 LDCM0580  Fragment21 Ramos C170(0.65); C234(0.61)  LDD2195  [23]
 LDCM0582  Fragment23 Ramos C170(0.52); C234(0.81)  LDD2196  [23]
 LDCM0578  Fragment27 Ramos C170(0.67); C234(0.50)  LDD2197  [23]
 LDCM0586  Fragment28 Ramos C170(0.85); C234(0.70)  LDD2198  [23]
 LDCM0588  Fragment30 Ramos C234(0.84)  LDD2199  [23]
 LDCM0589  Fragment31 Ramos C234(0.64)  LDD2200  [23]
 LDCM0590  Fragment32 Ramos C170(1.10)  LDD2201  [23]
 LDCM0468  Fragment33 HCT 116 C170(0.99)  LDD0785  [8]
 LDCM0566  Fragment4 Ramos C170(1.55); C234(0.85)  LDD2184  [23]
 LDCM0427  Fragment51 HCT 116 C170(0.97); C234(1.82)  LDD0744  [8]
 LDCM0614  Fragment56 Ramos C170(0.81); C234(0.28)  LDD2205  [23]
 LDCM0569  Fragment7 Ramos C234(0.47)  LDD2186  [23]
 LDCM0571  Fragment9 Ramos C170(1.40)  LDD2188  [23]
 LDCM0116  HHS-0101 DM93 Y92(0.80)  LDD0264  [7]
 LDCM0117  HHS-0201 DM93 Y92(0.55)  LDD0265  [7]
 LDCM0118  HHS-0301 DM93 Y92(0.78)  LDD0266  [7]
 LDCM0119  HHS-0401 DM93 Y92(0.65)  LDD0267  [7]
 LDCM0120  HHS-0701 DM93 Y92(1.62)  LDD0268  [7]
 LDCM0123  JWB131 DM93 Y92(2.98)  LDD0285  [6]
 LDCM0125  JWB146 DM93 Y92(0.48)  LDD0287  [6]
 LDCM0126  JWB150 DM93 Y92(0.69)  LDD0288  [6]
 LDCM0127  JWB152 DM93 Y92(0.47)  LDD0289  [6]
 LDCM0129  JWB202 DM93 Y92(0.55)  LDD0291  [6]
 LDCM0130  JWB211 DM93 Y92(2.38)  LDD0292  [6]
 LDCM0022  KB02 HCT 116 C170(1.70)  LDD0080  [8]
 LDCM0023  KB03 HCT 116 C170(1.80)  LDD0081  [8]
 LDCM0024  KB05 HCT 116 C170(1.90)  LDD0082  [8]
 LDCM0006  Micheliolide M9-ENL1 1.70  LDD0050  [4]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C170(0.87)  LDD2125  [3]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C170(1.02)  LDD2140  [3]
 LDCM0019  Staurosporine Hep-G2 N.A.  LDD0083  [21]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone acetyltransferase KAT5 (KAT5) MYST (SAS/MOZ) family Q92993
Serine/threonine-protein phosphatase 2A 65 kDa regulatory subunit A alpha isoform (PPP2R1A) Phosphatase 2A regulatory subunit A family P30153
Serine/threonine-protein kinase VRK1 (VRK1) CK1 Ser/Thr protein kinase family Q99986
Septin-1 (SEPTIN1) Septin GTPase family Q8WYJ6
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hsp90 co-chaperone Cdc37 (CDC37) CDC37 family Q16543
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Other
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Borealin (CDCA8) Borealin family Q53HL2
GAS2-like protein 3 (GAS2L3) GAS2 family Q86XJ1
Histone H3.1t (H3-4) Histone H3 family Q16695
Baculoviral IAP repeat-containing protein 5 (BIRC5) IAP family O15392
Inner centromere protein (INCENP) INCENP family Q9NQS7
Microtubule-associated protein RP/EB family member 1 (MAPRE1) MAPRE family Q15691
Nucleophosmin (NPM1) Nucleoplasmin family P06748

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Hesperidin Small molecular drug DB04703
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pha-739358 Small molecular drug D02RJY
Investigative
Click To Hide/Show 25 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isis 173813 Antisense drug D0K1JI
Isis 173831 Antisense drug D0PI2A
Isis 173840 Antisense drug D0Y5UO
Isis 173848 Antisense drug D07PVS
4-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]Pyridine Small molecular drug D04MYT
6-bromoindirubin-3-oxime Small molecular drug D06OAH
7-bromoindirubin-3-oxime Small molecular drug D0L1GF
7-chloroindirubin-3-oxime Small molecular drug D0K8YI
7-fluoroindirubin-3-acetoxime Small molecular drug D0I1IK
7-fluoroindirubin-3-oxime Small molecular drug D00TKJ
7-iodoindirubin-3-oxime Small molecular drug D0K6VW
At9283 Small molecular drug DB05169
Cgp-57380 Small molecular drug D0A7FQ
Enzastaurin Small molecular drug DB06486
Hesperadin Small molecular drug D05WSM
Indirubin-3'-monoxime Small molecular drug D0Y0ES
Indirubin-3-acetoxime Small molecular drug D06AGN
Indirubin-3-methoxime Small molecular drug D0V6LP
Pmid16451062c46 Small molecular drug D06LJL
Pmid20855207c25 Small molecular drug D0ME9B
Pmid21742770c1 Small molecular drug D01TDV
Quinazoline Deriv. 1 Small molecular drug D0U8VY
Reversine Small molecular drug DB07340
Su 6656 Small molecular drug D0CE3R
Tak-901 Small molecular drug DB12756

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 Comprehensive Structure-Activity Profiling of Micheliolide and its Targeted Proteome in Leukemia Cells via Probe-Guided Late-Stage C-H Functionalization. ACS Cent Sci. 2021 May 26;7(5):841-857. doi: 10.1021/acscentsci.0c01624. Epub 2021 Apr 28.
Mass spectrometry data entry: PXD024455
5 Chemoproteomic Profiling Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function. Mol Pharm. 2018 Jun 4;15(6):2413-2422. doi: 10.1021/acs.molpharmaceut.8b00250. Epub 2018 May 15.
6 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
7 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
8 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
9 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
10 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
11 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
12 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
13 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
14 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
15 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
16 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
17 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
18 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
19 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
20 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
21 Comprehensive identification of staurosporine-binding kinases in the hepatocyte cell line HepG2 using Capture Compound Mass Spectrometry (CCMS). J Proteome Res. 2010 Feb 5;9(2):806-17. doi: 10.1021/pr9007333.
22 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
23 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578